Phosphoramidate derivatives of acyclovir: Synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro

作者：Zakirova Natalia F^*; Shipitsyn Alexander V; Jasko Maxim V; Prokofjeva Maria M; Andronova Valeria L; Galegov Georgiy A; Prassolov Vladimir S; Kochetkov Sergey N

来源：Bioorganic & Medicinal Chemistry, 2012, 20(19): 5802-5809.

DOI：10.1016/j.bmc.2012.08.008

• Phosphoramidates
• Acyclovir (ACV)
• Antiviral activity
• Herpes Simplex Virus (HSV)
• Human Immunodeficiency Virus (HIV)

The antiviral activity against HIV and HSV and the chemical stability of ACV phosphoramidate derivatives were studied. The phosphoramidates of ACV demonstrated moderate activity. The best compound appeared to be 9-(2-hydroxymethyl)guanine phosphoromonomorpholidate (7), which inhibited virus replication in pseudo-HIV-1 particles by 50% at 50 mu M. It also inhibited replication of wild-type HSV-1 (9.7 mu M) as well as an acyclovir-resistant strain (25 mu M). None of the synthesised compounds showed any cytotoxicity.

• 出版日期2012-10-1